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Int J Parasitol Drugs Drug Resist. 2017 Apr;7(1):120-129. doi: 10.1016/j.ijpddr.2017.02.002. Epub 2017 Feb 21.

4-Nitro styrylquinoline is an antimalarial inhibiting multiple stages of Plasmodium falciparum asexual life cycle.

Author information

1
Division of Molecular Microbiology, Burnett School of Biomedical Sciences, College of Medicine, University of Central Florida, Orlando, FL, USA.
2
Department of Chemistry, University of Central Florida, Orlando, FL, USA.
3
Institut Pasteur Korea, Seongnam-si, Gyeonggi-do, South Korea.
4
Center Pasteur, Yaounde, Cameroon.
5
Division of Molecular Microbiology, Burnett School of Biomedical Sciences, College of Medicine, University of Central Florida, Orlando, FL, USA. Electronic address: dchak@ucf.edu.

Abstract

Drugs against malaria are losing their effectiveness because of emerging drug resistance. This underscores the need for novel therapeutic options for malaria with mechanism of actions distinct from current antimalarials. To identify novel pharmacophores against malaria we have screened compounds containing structural features of natural products that are pharmacologically relevant. This screening has identified a 4-nitro styrylquinoline (SQ) compound with submicromolar antiplasmodial activity and excellent selectivity. SQ exhibits a cellular action distinct from current antimalarials, acting early on malaria parasite's intraerythrocytic life cycle including merozoite invasion. The compound is a fast-acting parasitocidal agent and also exhibits curative property in the rodent malaria model when administered orally. In this report, we describe the synthesis, preliminary structure-function analysis, and the parasite developmental stage specific action of the SQ scaffold.

KEYWORDS:

Antimalarials; Antiplasmodials; Invasion inhibitor; Natural-product-like compounds; Styrylquinoline

PMID:
28285258
PMCID:
PMC5350499
DOI:
10.1016/j.ijpddr.2017.02.002
[Indexed for MEDLINE]
Free PMC Article

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